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Titolo:
SUBSTANCE P-EVOKED CALCIUM MOBILIZATION AND IONIC CURRENT ACTIVATION IN THE HUMAN ASTROCYTOMA CELL-LINE U-373-MG - PHARMACOLOGICAL CHARACTERIZATION
Autore:
PRADIER L; HEUILLET E; HUBERT JP; LAVILLE M; LEGUERN S; DOBLE A;
Indirizzi:
CTR RECH VITRY ALFORTVILLE,RHONE POULENC RORER BIOL DEPT,13 QUAI JULES GUESDE F-94403 VITRY FRANCE
Titolo Testata:
Journal of neurochemistry
fascicolo: 5, volume: 61, anno: 1993,
pagine: 1850 - 1858
SICI:
0022-3042(1993)61:5<1850:SPCMAI>2.0.ZU;2-1
Fonte:
ISI
Lingua:
ENG
Soggetto:
DORSAL HORN NEURONS; INOSITOL PHOSPHOLIPID HYDROLYSIS; CEREBRAL CORTICAL SLICES; GUINEA-PIG ILEUM; SPECIES-DIFFERENCES; NEUROKININ-1 RECEPTORS; INTRACELLULAR CALCIUM; NONPEPTIDE ANTAGONIST; TACHYKININ RECEPTORS; SELECTIVE AGONISTS;
Keywords:
HUMAN NK(1) TACHYKININ RECEPTOR; U-373-MG CELL LINE; NK(1) SELECTIVE ANTAGONISTS; PATCH CLAMP; INTRACELLULAR CALCIUM; RP-67580; CP-96,345;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
58
Recensione:
Indirizzi per estratti:
Citazione:
L. Pradier et al., "SUBSTANCE P-EVOKED CALCIUM MOBILIZATION AND IONIC CURRENT ACTIVATION IN THE HUMAN ASTROCYTOMA CELL-LINE U-373-MG - PHARMACOLOGICAL CHARACTERIZATION", Journal of neurochemistry, 61(5), 1993, pp. 1850-1858

Abstract

In the human astrocytoma cell line U 373 MG, application of substanceP (SP) leads to a transient increase in cytosolic calcium concentration and to a biphasic current response in voltage-clamped cells. Using these two functional assays we have characterized pharmacologically the SP response in U 373 MG cells. SP and [L-Pro9]SP displayed high potencies in both assays with EC50 values of 2.5 X 10(-9) M and 1 X 10(-9)M on calcium responses and 1 X 10(-9) M and 5 X 10(-9) M on ion current responses, respectively. The high potency of SP and [L-Pro9]SP as well as the low potency of [LyS5,MeLeu9,N-Leu10]neurokinin A(4-10) and the inactivity of senktide demonstrate the NK1-type pharmacology of these responses. Furthermore, the NK, antagonists (+/-)-CP 96,345, its chloro analogue, -3-(2-chlorobenzylamino)-2-benzhydrylquinuclidine, andRP 67580 were potent antagonists of both SP responses. For the calcium mobilization induced by Sp(10(-7) M), the IC50 values for the three antagonists were 4 X 10(-10) M, 4 X 10(-9) M, and 9 X 10(-9) M, respectively, whereas on the current response evoked by SP (10(-8) M), the IC50 values were 8 x 10(-9) M, 2.4 x 10(-8) M, and 1.2 x 10(-7) M, respectively. Despite differences in the absolute IC50 values obtained with both techniques, the relative potencies of the three antagonists correlate fairly well. The U 373 MG cell line provides a useful model system for studies of the pharmacology of the human NK1 receptor and its transduction mechanisms at the level of second messengers and modulation of ion currents.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 27/11/20 alle ore 21:18:24